Aryl thioxanthines

Details Aryl thioxanthines Aryl thioxanthines

C - Chemistry, Metallurgy

07

D

C07D 473/22 (2006.01) A61K 31/52 (2006.01) C07D 473/18 (2006.01)

Patent

CA 2206287

Disclosed are compounds having formula (I) or (II), wherein: Q3, Q6a, Q6b and Q8 are independently a bond, C1-8 alkylene, C2-8 alkenylene and C2-8 alkynylene, and R3, R6a, R6b and R8 are independently hydrogen, aryl or heteroaryl, optionally substituted by halogen, hydroxy, alkoxy, nitro, cyano and carboxy, provided that: Q3R3 is not hydrogen or methyl in formula (I) or (II); and at least one of R3 and R8 is aryl or heteroaryl in formula (I). The compounds are effective PDE IV inhibitors and possess improved PDE IV inhibition and improved selectivity with regard to PDE III inhibition.

L'invention concerne des composés répondant aux formules (I) ou (II). Dans lesdites formules, Q¿3?, Q¿6a?, Q¿6b? et Q¿8? sont indépendamment une liaison, C¿1-8? alkylène, C¿2-8? alcénylène et C¿2-8? alcynylène, et R¿3?, R¿6a?, R¿6b? et R¿8? sont indépendamment hydrogène, aryle ou hétéroaryle, éventuellement substitués par halogène, hydroxy, alcoxy, nitro, cyano et carboxy, à condition que Q¿3?R¿3? ne soit ni hydrogène ni méthyle dans les formules (I) ou (II); et que R¿3? et/ou R¿8? soi(en)t aryle ou hétéroaryle dans la formule (I). Les composés considérés sont des inhibiteurs efficaces des phosphodiestérases (PDE) IV et ont une capacité d'inhibition améliorée par rapport aux PDE IV ainsi qu'une sélectivité améliorée par rapport à l'inhibition des PDE III.

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